Open AccessStudies on 5-fluoro-.ALPHA.-methyltryptamine and p-chloro-.BETA.-methylphenethylamine: Determination of the MAO-A or MAO-B selective inhibition in vitro.
Author(s) -
Hiroyasu Kinemuchi,
Yasuhiko Arai,
Yoshie Toyoshima,
Takeshi Tadano,
Kensuke Kisara
Publication year - 1988
Publication title -
japanese journal of pharmacology/japanese journal of pharmacology
Language(s) - English
Resource type - Journals
eISSN - 1347-3506
pISSN - 0021-5198
DOI - 10.1254/jjp.46.197
Subject(s) - in vitro , in vivo , non competitive inhibition , chemistry , stereochemistry , alpha (finance) , inhibitory postsynaptic potential , pharmacology , biochemistry , enzyme , biology , medicine , surgery , construct validity , microbiology and biotechnology , patient satisfaction
To further clarify highly MAO-A- or -B-selective inhibitory properties of 5-fluoro-alpha-methyltryptamine (5-FMT) and p-chloro-beta-methylphenethylamine (p-CMPEA), we determined the types and K1 values of inhibition of rat brain MAO-A and -B activity in vitro. The kinetic data obtained showed that 5-FMT is a competitive MAO-A-selective inhibitor with about a 18,000-fold higher sensitivity than MAO-B. In contrast, p-CMPEA is a competitive MAO-B-selective inhibitor with about a 620-fold higher sensitivity. Based on the present findings of highly MAO-A- or -B-selective inhibition, these two compounds might prove to be of value in in vivo studies.